SML0385

ML218

≥98% (HPLC)

• Sinónimos: 3,5-Dichloro-N-[[(1α,5α,6-exo,6α)-3-(3,3-dimethylbutyl)-3-azabicyclo[3.1.0]hex-6-yl]methyl]benzamide, CID 45115620, VU0413807, VU0424199-1
• Fórmula empírica (notación de Hill): C₁₉H₂₆Cl₂N₂O
• Número de CAS: 1346233-68-8
• Peso molecular: 369.33
• Código UNSPSC: 12352200
• ID de la sustancia en PubChem: 329825385
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥98% (HPLC)
• Formulario: powder
• color: white to beige
• solubilidad: DMSO: 10 mg/mL (clear solution)
• temp. de almacenamiento: 2-8°C
• cadena SMILES: CC(C)(C)CCN1C[C@H]2C(CNC(=O)c3cc(Cl)cc(Cl)c3)[C@H]2C1
• InChI: 1S/C19H26Cl2N2O/c1-19(2,3)4-5-23-10-16-15(17(16)11-23)9-22-18(24)12-6-13(20)8-14(21)7-12/h6-8,15-17H,4-5,9-11H2,1-3H3,(H,22,24)/t15-,16-,17+
• Clave InChI: GSJIGYLGKSBYBC-OSYLJGHBSA-N

Descripción

Aplicación

ML218 has been used as a:

• T-type channel blocker to test its effect on the nociceptive behavior associated with homocysteinemia rats[1]
• T-type voltage-sensitive calcium channel (VSCC) inhibitor in osteoblasts[2]
• T-type calcium channel blocker to test its effect on the viability of neural progenitor cells[3]

Acciones bioquímicas o fisiológicas

ML218 (CID 45115620) is a potent and selective T-Type (Cav3.1, Cav3.2, Cav3.3) calcium channel inhibitor (Cav3.2, IC50 = 150 nM in Ca2+ flux; Cav3.2 IC50 = 310 nM and Cav3.3 IC50 = 270 nM with good Drug metabolism/Pharmacokinetics. In a panel of 68 GPCRs, ion channels and transporters, ML218 was found to bind significantly only two other targets (sodium channel site 2 and sigma 1) and had no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. It showed robust inhibition of calcium current in STN neurons and was orally active in a rodent model of Parkinson′s Disease.

ML218 is a potent, selective T-Type calcium channel inhibitor.

Características y beneficios

This compound is featured on the Calcium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable